Acylamino-Directed Specific Sequential Difunctionalizations of Anilides via Metal-Free Relay Reactions for p-Oxygen and o-Nitrogen Incorporation
摘要:
Novel acylamino-directed relay disubstitutions realize the sequential difunctionalizations of anilides (1) under mild and metal-free conditions for the first time. This [bis(trifluoroacetoxy)iodo]benzene (PIFA) and BF3 center dot Et2O promoted straightforward reaction produces a series of p-acetoxyl- or p-alkoxyl-o-nitro-N-arylamides (2), which are key scaffolds of various drugs, functional materials, and bioactive molecules. The flexibility with respect to the functional groups in these products affords this novel protocol excellent versatility for synthetic applications.
Rapid one-pot preparation of 2-substituted benzimidazoles from 2-nitroanilines using microwave conditions
作者:David S. VanVliet、Paul Gillespie、Jan J. Scicinski
DOI:10.1016/j.tetlet.2005.07.130
日期:2005.9
A high yielding one-pot procedure for the generation of 2-substituted benzimidazoles directly from 2-nitroanilines by in situ reduction and cyclization using a microwave procedure is described.
O-pyridinequinone derivatives, the composition containing the derivatives, the process for preparation of the derivatives and the use of the derivatives
申请人:Gu Lianquan
公开号:US20060111405A1
公开(公告)日:2006-05-25
The present invention relates to the o-pyridinequinone disubstituted derivatives, the composition containing the derivatives, the process for preparation of the derivatives and the use of the derivatives. The o-pyridinequinone disubstituted derivatives of the present invention have action of selectivity inhibiting COX-2 and they can be made into pharmaceuticals. The o-pyridinequinone disubstituted derivatives of the present invention have no acute toxicities and are a safe pharmaceutical.